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1. WO2018139438 - PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINEAMIDE COMPOUND

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Publication Number WO/2018/139438
Publication Date 02.08.2018
International Application No. PCT/JP2018/001927
International Filing Date 23.01.2018
IPC
C07D 207/16 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
10with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4439 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/496 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 13/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 37/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
A61P 37/08 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
CPC
A61K 31/4439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/496
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
A61P 37/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
A61P 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
Applicants
  • アステラス製薬株式会社 ASTELLAS PHARMA INC. [JP]/[JP]
Inventors
  • 中島　豊 NAKAJIMA, Yutaka
  • ▲今▼田　直 IMADA, Sunao
  • 山本　永利子 YAMAMOTO, Eriko
  • 土屋　和之 TSUCHIYA, Kazuyuki
  • 原山　悠 HARAYAMA, Yu
  • 松本　俊一郎 MATSUMOTO, Shunichiro
Agents
  • 鈴木　▲頼▼子 SUZUKI, Yoriko
  • 鈴木　▲頼▼子 SUZUKI, Yoriko
  • 濱井　康丞 HAMAI, Kousuke
  • 寺内　輝和 TERAUCHI, Terukazu
  • 飯室　加奈 IIMURO, Kana
  • 影山　路人 KAGEYAMA, Michihito
  • 川濱　周弥 KAWAHAMA, Shuya
  • 鎌田　啓明 KAMADA, Hiroaki
Priority Data
2017-01032124.01.2017JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINEAMIDE COMPOUND
(FR) COMPOSÉ DE PROLINEAMIDE SUBSTITUÉ PAR UN PHÉNYLDIFLUOROMÉTHYLE
(JA) フェニルジフルオロメチル置換プロリンアミド化合物
Abstract
(EN) [Problem] To provide a compound useful as a cathepsin S inhibitor. [Solution] The present inventors have studied on a compound which has a cathepsin S-inhibiting activity and can be used as an active ingredient for a pharmaceutical composition for preventing and/or treating an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis, an allergy, or organ, bone marrow or tissue graft rejection. As a result, it has been confirmed that a phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity. This confirmation leads to the accomplishment of the present invention. The phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity, and can be used as a prophylactic and/or therapeutic agent for an autoimmune disease such as SLE and nephritis, an allergy, or organ, bone marrow or tissue graft rejection.
(FR) Le problème décrit par la présente invention est de produire un composé destiné à être utilisé en tant qu'inhibiteur de la cathepsine S. La solution de l'invention porte sur un composé qui possède une activité d'inhibition de la cathepsine S et qui peut être utilisé en tant que principe actif pour une composition pharmaceutique pour prévenir et/ou traiter une maladie auto-immune telle qu'un lupus érythémateux disséminé (LED) et une néphrite lupique, une allergie, ou un organe, une moelle osseuse ou un rejet de greffe de tissu. Par conséquent, il a été confirmé qu'un composé de prolineamide substitué par un phényldifluorométhyle selon la présente invention possède une activité d'inhibition de la cathepsine S. Cette confirmation a conduit à la mise au point de la présente invention. Le composé de prolineamide substitué par un phényldifluorométhyle selon la présente invention possède une activité d'inhibition de la cathepsine S, et peut être utilisé en tant qu'agent prophylactique et/ou thérapeutique pour une maladie auto-immune telle qu'un LED et une néphrite, une allergie, ou pour un organe, une moelle osseuse ou un rejet de greffe de tissu.
(JA) 【課題】カテプシンＳ阻害剤として有用な化合物を提供する。 【解決手段】本発明者らは、カテプシンＳ阻害作用を有し、全身性エリテマトーデス（ＳＬＥ）やループス腎炎を含む自己免疫疾患、アレルギー、又は、臓器、骨髄若しくは組織の移植片拒絶の予防及び／又は治療用医薬組成物の有効成分となりうる化合物について検討し、本発明のフェニルジフルオロメチル置換プロリンアミド化合物がカテプシンＳ阻害作用を有することを確認し、本発明を完成した。本発明のフェニルジフルオロメチル置換プロリンアミド化合物は、カテプシンＳ阻害作用を有し、ＳＬＥや腎炎を含む自己免疫疾患、アレルギー、又は、臓器、骨髄若しくは組織の移植片拒絶の予防及び／又は治療剤として使用できる。
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